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13 条记录 (耗时 0.051 秒)

    Novel-prodrugs for phosphorus-containing compounds
    1.
    发明申请
    Novel-prodrugs for phosphorus-containing compounds 有权

    公开(公告)号：US20050288240A1

    公开(公告)日：2005-12-29

    申请号：US11145194

    申请日：2005-06-03

    申请人： Mark Erion ,  K. Reddy ,  Edward Robinson ,  Bheemarao Ugarkar

    发明人： Mark Erion ,  K. Reddy ,  Edward Robinson ,  Bheemarao Ugarkar

    IPC分类号： A61K31/7056 ,  A61K31/7072 ,  A61K31/7076 ,  C07F9/6571 ,  C07F9/6574 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207

    CPC分类号： C07H19/10 ,  A61K31/7056 ,  A61K31/7072 ,  A61K31/7076 ,  C07F9/657154 ,  C07F9/657181 ,  C07F9/65742 ,  C07F9/65744 ,  C07H19/20 ,  C07H19/207 ,  Y02A50/411

    摘要： Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described: wherein: V, W, and W′ are independently selected from the group consisting of —H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, and 1-alkynyl; or together V and Z are connected via an additional 3-5 atoms to form a cyclic group containing 5-7 atoms, optionally 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from both O groups attached to the phosphorus; or together V and Z are connected via an additional 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the O attached to the phosphorus; together V and W are connected via an additional 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from the group consisting of hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to one of said carbon atoms that is three atoms from an O attached to the phosphorus; together Z and W are connected via an additional 3-5 atoms to form a cyclic group, optionally containing one heteroatom, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; together W and W′ are connected via an additional 2-5 atoms to form a cyclic group, optionally containing 0-2 heteroatoms, and V must be aryl, substituted aryl, heteroaryl, or substituted heteroaryl; Z is selected from the group consisting of —CHR2OH, —CHR2OC(O)R3, —CHR2OC(S)R3, —CHR2OC(S)OR3, —CHR2OC(O)SR3, —CHR2OCO2R3, —OR2, —SR2, —CHR2N3, —CH2aryl, —CH(aryl)OH, —CH(CH═CR22)OH, —CH(C≡CR2)OH, —R2, —NR22, —OCOR3, —OCO2R3, —SCOR3, —SCO2R3, —NHCOR2, —NHCO2R3, —CH2NHaryl, —(CH2)p—OR12, and —(CH2)p—SR12; p is an integer 2 or 3; with the provisos that: a) V, Z, W, W′ are not all —H; and b) when Z is —R2, then at least one of V, W, and W′ is not —H, alkyl, aralkyl, or alicyclic; R2 is selected from the group consisting of R3 and —H; R3 is selected from the group consisting of alkyl, aryl, alicyclic, and aralkyl; R12 is selected from the group consisting of —H, and lower acyl; M is selected from the group that attached to PO32−, P2O63−, or P3O94− is a biologically active agent, and is attached to the phosphorus in formula I via a carbon, oxygen, sulfur or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof.

    Novel 2'-C-methyl nucleoside derivatives
    4.
    发明申请
    Novel 2'-C-methyl nucleoside derivatives 有权
    新型2'-C-甲基核苷衍生物

    公开(公告)号：US20070042989A1

    公开(公告)日：2007-02-22

    申请号：US11589363

    申请日：2006-10-30

    申请人： K. Reddy ,  Mark Erion

    发明人： K. Reddy ,  Mark Erion

    IPC分类号： A61K31/7076 ,  C07H19/00 ,  A61K38/21

    CPC分类号： C07H19/04 ,  C07H19/20

    摘要： Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:

    摘要翻译： 描述了式I化合物，立体异构体及其药学上可接受的盐或前药，其制备方法及其用于治疗丙型肝炎病毒感染的用途：

    Novel 2'-C-methyl nucleoside derivatives
    8.
    发明申请
    Novel 2'-C-methyl nucleoside derivatives 审中-公开
    新型2'-C-甲基核苷衍生物

    公开(公告)号：US20050182252A1

    公开(公告)日：2005-08-18

    申请号：US10903215

    申请日：2004-07-29

    申请人： K. Reddy ,  Mark Erion

    发明人： K. Reddy ,  Mark Erion

    IPC分类号： C07H19/04 ,  C07H19/20

    CPC分类号： C07H19/04 ,  C07H19/20

    摘要： Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:

    摘要翻译： 描述了式I化合物，立体异构体及其药学上可接受的盐或前药，其制备方法及其用于治疗丙型肝炎病毒感染的用途：

    Prodrugs for liver specific drug delivery
    9.
    发明申请
    Prodrugs for liver specific drug delivery 有权
    用于肝脏特异性药物递送的前药

    公开(公告)号：US20050101775A1

    公开(公告)日：2005-05-12

    申请号：US10844747

    申请日：2004-05-12

    申请人： Mark Erion ,  K. Reddy

    发明人： Mark Erion ,  K. Reddy

    IPC分类号： A61K31/661 ,  A61K31/664 ,  A61K49/00 ,  A61P3/06 ,  A61P3/10 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P33/10 ,  A61P35/00 ,  C07F9/28 ,  C07F9/547 ,  C07F9/6571 ,  C07F9/6584 ,  C07H15/252 ,  C07H15/26

    CPC分类号： C07F9/657118 ,  C07F9/657127 ,  C07F9/657154 ,  C07F9/65846 ,  C07H15/252 ,  C07H15/26

    摘要： The present invention is directed towards novel cyclic phosph(oramid)ate prodrugs of alcohol-, amine-, and thiol-containing drugs, their preparation, their synthetic intermediates, and their uses. Another aspect of the invention is the use of the prodrugs to treat diseases that benefit from enhanced drug distribution to the liver and like tissues and cells that express cytochrome P450, including hepatitis, cancer, liver fibrosis, malaria, other viral and parasitic infections, and metabolic diseases where the liver is responsible for the overproduction of the biochemical end product, e.g. glucose (diabetes); cholesterol, fatty acids and triglycerides (hyperlipidemia) (atherosclerosis) (obesity). In one aspect, the invention is directed towards the use of the prodrugs to enhance oral drug delivery. In another aspect, the prodrugs are used to prolong pharmacodynamic half-life of the drug. In addition, the prodrug methodology of the current invention is used to achieve sustained delivery of the parent drug. In another aspect, the prodrugs are used to increase the therapeutic index of the drug. In another aspect of the invention, a method of making these prodrugs is described. In another aspect, the prodrugs are also useful in the delivery of diagnostic imaging agents to the liver.

    摘要翻译： 本发明涉及新型环状磷酸酯（oramid），其包含醇，胺和硫醇的药物，其制备方法，其合成中间体及其用途。 本发明的另一方面是使用前药治疗受益于增强的药物分布到肝脏和表达细胞色素P450的组织和细胞（包括肝炎，癌症，肝纤维化，疟疾，其他病毒和寄生虫感染）的细胞的疾病，以及 肝脏负责生化终产物过度生成的代谢性疾病，例如， 葡萄糖（糖尿病）; 胆固醇，脂肪酸和甘油三酯（高脂血症）（动脉粥样硬化）（肥胖）。 一方面，本发明涉及前药用于增强口服药物递送的用途。 另一方面，前药用于延长药物的药效半衰期。 此外，本发明的前药方法用于实现母体药物的持续递送。 在另一方面，前药用于增加药物的治疗指数。 在本发明的另一方面，描述了制备这些前药的方法。 在另一方面，前药还可用于将诊断成像剂递送至肝脏。